Cholecalciferol derivatives

A - Human Necessities – 61 – K

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A61K 31/59 (2006.01) C07C 33/44 (2006.01) C07C 45/30 (2006.01) C07C 49/743 (2006.01) C07C 401/00 (2006.01) C07F 7/18 (2006.01)

Patent

CA 1286693

ABSTRACT The novel .DELTA.22- or .DELTA.23 -26,26,26,27,27,27-hexa- fluoro-1.alpha.,25-dihydroxycholecalciferol has vitamin D acti- vity. It can be prepared by reacting [1R-[1.beta.(R*),3a.alpha.,- 4.beta.,7a.beta.]]-octahydro-1-[6,6,6 -trifluoro-5-trimethylsilyloxy]- -5-trifluoromethyl-1-methyl -2-hexenyl]-7a-methyl-1H-inden- -4-one or [1R-[1.beta.(R*),3a.alpha.,4.beta.,7a.beta.]]-octahydro-1-[6,6,6-tri- fluoro -5-trimethylsilyloxy-5-trifluoromethyl-1-methyl -3-hexenyl]-7a-methyl-1H-inden-4-one, respectively, with [3S-(3.alpha.,5.beta.,Z)]-2-[2-methylene-3,5 -bis[(1,1-dimethyl- ethyl)dimethylsilyloxy]cyclohexylidene]ethyldiphenyl phos- phine oxide and removing the silyl protecting groups.

495246

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